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Title

Asymmetric Synthesis of Pochonin E and F, Revision of Their Proposed Structure, and Their Conversion to Potent Hsp90 Inhibitors

Authors
Karthikeyan, Ganesan
Barluenga, Sofia
Zoete, Vincent
Karplus, Martin
Published in Chemistry - A European Journal. 2012, vol. 18, no. 29, p. 8978-8986
Abstract A concise and modular synthesis of pochonin E and F, and their epimers at C-6 established the correct stereochemistry of these two natural products. Several members of the pochonin family have been shown to bind the heat shock protein 90 (Hsp90), which has been the focus of intense drug discovery efforts. Pochonin E and F as well as their epimers were derivatized into the corresponding pochoximes and further modified at the C-6 position. Molecular dynamics simulations, docking studies, and Hsp90 affinity measurements were performed to evaluate the impact of these modifications.
Keywords conformation analysisHsp90inhibitorslactonespochonins
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Other version: http://doi.wiley.com/10.1002/chem.201200546
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KARTHIKEYAN, Ganesan et al. Asymmetric Synthesis of Pochonin E and F, Revision of Their Proposed Structure, and Their Conversion to Potent Hsp90 Inhibitors. In: Chemistry - A European Journal, 2012, vol. 18, n° 29, p. 8978-8986. https://archive-ouverte.unige.ch/unige:24669

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Deposited on : 2012-12-17

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